Conserved Protein Domain Family
PI3Kc_IA_delta

?
cd05174: PI3Kc_IA_delta 
Phosphoinositide 3-kinase (PI3K), class IA, delta isoform, catalytic domain; The PI3K catalytic domain family is part of a larger superfamily that includes the catalytic domains of other kinases such as the typical serine/threonine/tyrosine protein kinases (PKs), aminoglycoside phosphotransferase, choline kinase, and RIO kinases. PI3Ks catalyze the transfer of the gamma-phosphoryl group from ATP to the 3-hydroxyl of the inositol ring of D-myo-phosphatidylinositol (PtdIns) or its derivatives. PI3Ks can be divided into three main classes (I, II, and III), defined by their substrate specificity, regulation, and domain structure. Class I PI3Ks are the only enzymes capable of converting PtdIns(4,5)P2 to the critical second messenger PtdIns(3,4,5)P3. Class I enzymes are heterodimers and exist in multiple isoforms consisting of one catalytic subunit (out of four isoforms) and one of several regulatory subunits. They are further classified into class IA (alpha, beta and delta) and IB (gamma). Class IA enzymes contain an N-terminal p85 binding domain, a Ras binding domain, a lipid binding C2 domain, a PI3K homology domain of unknown function, and a C-terminal ATP-binding cataytic domain. They associate with a regulatory subunit of the p85 family and are activated by tyrosine kinase receptors. PI3Kdelta is mainly expressed in immune cells and plays an important role in cellular and humoral immunity. It plays a major role in antigen receptor signaling in B-cells, T-cells, and mast cells. It regulates the differentiation of peripheral helper T-cells and controls the development and function of regulatory T-cells.
BioAssay Targets and Results
?
CID: 44124863
AID: 616089
GI: 67477424
IC50: 0.0008µM
more
Inhibition of human N-terminal His-tagged PI3Kdelta expressed in insect Sf9 cells using PI(4,5)P2 as substrate after 20 mins by alphascreen assay in presence of 8 uM ATP
Target Name: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Chemical Name: CHEMBL1822054
IC50: 0.0008µM
CID: 50990924
AID: 595401
GI: 67477424
IC50: 0.0012µM
more
Inhibition of human PI3Kdelta expressed in Sf9 cells
Target Name: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Chemical Name: CHEMBL1615189
IC50: 0.0012µM
CID: 22036885
AID: 626771
GI: 67477424
IC50: 0.00065µM
more
Inhibition of human His-tagged PI3K p110delta after 2 hrs by HTRF assay
Target Name: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Chemical Name: SureCN374947
IC50: 0.00065µM
Statistics
?
PSSM-Id: 119434
View PSSM: cd05174
Aligned: 3 rows
Threshold Bit Score: 774.611
Threshold Setting Gi: 41055186
Created: 9-Aug-2007
Updated: 17-Jan-2013
Structure
?
Aligned Rows:
Hierarchy
?
Display:
 
Feature 1:ATP binding site [chemical binding site]
Evidence:

cd05174 is part of a hierarchy of related CD models.
Use the graphical representation to navigate this hierarchy.
cd00142:PI3Kc_likecd00891:PI3Kccd00892:PIKKc_ATRcd00893:PI4Kc_IIIcd00894:PI3Kc_IB_gammacd00895:PI3Kc_C2_betacd00896:PI3Kc_IIIcd05163:PIKK_TRRAPcd05164:PIKKccd05165:PI3Kc_Icd05166:PI3Kc_IIcd05167:PI4Kc_III_alphacd05168:PI4Kc_III_betacd05169:PIKKc_TORcd05170:PIKKc_SMG1cd05171:PIKKc_ATMcd05172:PIKKc_DNA-PKcd05173:PI3Kc_IA_betacd05174:PI3Kc_IA_deltacd05175:PI3Kc_IA_alphacd05176:PI3Kc_C2_alphacd05177:PI3Kc_C2_gamma199232894105518660593018199232894105518660593018
cd05174 Sequence Cluster
cd05174 Sequence Cluster
Sub-family Hierarchy
Click to see CD Hierarchy help
 cd05174 Branch
 Whole Hierarchy
 [Download CDTree]
CD Hierarchy
Sequence Alignment
?
Format: Row Display: Color Bits: Type Selection:
                         10        20        30        40        50        60        70        80
                 ....*....|....*....|....*....|....*....|....*....|....*....|....*....|....*....|
Feature 1                                                                                 # ### #
gi 19923289  679 MKVLMKQGEALSKLKALNDFVKlssqktPKPQTKELMHLCMRQEAYLEaLSHLQSPLDPSTLLAEVCVEQCTFMDSKMKP 758
gi 41055186  679 IKSLMKQNEALNKMKALNDFVKsasqkaTRIQTTEDMKVCIKQETYMEaLSDVVSPLSPSIILCELCADKCKFMDSKMKP 758
gi 60593018  682 MKVLMKQGEALSKMKALNEFVKlsspkaTKPQAKEMMHVCMKQETYLEaLSHLQSPLNPSIILTEVCVDQCTFMDSKMKP 761
                         90       100       110       120       130       140       150       160
                 ....*....|....*....|....*....|....*....|....*....|....*....|....*....|....*....|
Feature 1                          # #  #                              #           ####    #  #  
gi 19923289  759 LWIMYSNeeagsggsVGIIFKNGDDLRQDMLTLQMIQLMDVLWKQEGLDLRMTPYGCLPTGDRTGLIEVVLRSDTIANIQ 838
gi 41055186  759 LWLMYKSky----dsVGIIFKNGDDLRQDMLTLQMIQIMDILWKTEGLDLRMQPYGCLSTGNKTGLIEVVKNSDTIANIQ 834
gi 60593018  762 LWIVFNNeetg-gggVGIIFKNGGDLRQDMLTLQMIQLMDVLWKQEGLDLRMTPYGCLSTGDKTGLIEVVMHSDTIANIQ 840
                        170       180       190       200       210       220       230       240
                 ....*....|....*....|....*....|....*....|....*....|....*....|....*....|....*....|
Feature 1                                                                   # #         ##       
gi 19923289  839 LNKSNmaataAFNKDALLNWLKSKNpgEALDRAIEEFTLSCAGYCVATYVLGIGDRHSDNIMIRESGQLFHIDFGHFLGN 918
gi 41055186  835 RNNSNsaataAFNKDALLNWLKSKNpgDKLDQAIEEFTLSCAGYCVATYVLGIGDRHSDNIMIRESGQLFHIDFGHFLGN 914
gi 60593018  841 LNKSNmaataAFNKDALLNWLKSKNpgDALEQAIEEFTLSCAGYCVATYVLGIGDRHSDNIMIRETGQLFHIDFGHFLGN 920
                        250       260       270       280       290       300       310       320
                 ....*....|....*....|....*....|....*....|....*....|....*....|....*....|....*....|
Feature 1                                                                                        
gi 19923289  919 FKTKFGINRERVPFILTYDFVHVIQQGktNNSEKFERFRGYCERAYTILRRHGLLFLHLFALMRAAGLPELscSKDIQYL 998
gi 41055186  915 FKSKFGINRERVPFILTYDFVHVIQEGrtNNSEKFERFRVCCEQAYKILCRNGTLFVNLFALMKAAGLPELnsSKDIQYL 994
gi 60593018  921 FKTKFGINRERVPFILTYDFVHVIQQGktNNSEKFERFRGYCEKAYMILRRHGPLFLHLFALMKAAGLPELtcSKDIQYL 1000
                        330       340       350       360
                 ....*....|....*....|....*....|....*....|..
Feature 1                                                  
gi 19923289  999 KDSLALgktEEEALKHFRVKFNEALRESWktKVNWLAHNVSK 1040
gi 41055186  995 KDSLALgksEEEALKNFKVKFNEALRESWktKVNWMMHTFAK 1036
gi 60593018 1001 KDSLALgktDEEALKHFRLKFNEALRESWktKVNWLAHNVSK 1042

| Disclaimer | Privacy statement | Accessibility |
NCBI Home NCBI Search NCBI SiteMap